Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Production process of chlorcyclizine hydrochloride

A kind of chlorocyclizine hydrochloride, production technology technology, applied in the field of drug synthesis, can solve the problems of harsh reaction conditions, pollution, many steps and the like

Inactive Publication Date: 2020-10-20
JIAOZUO FURUITANG PHARMA
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Wherein the cultural scientific name is: 1-(4-chloro-benzhydryl)-4-methylpiperazine hydrochloride; the production of chlorcyclizine hydrochloride mostly adopts synthetic methods, but various synthetic methods are prone to occur in the commonly used synthetic methods. Many problems, such as many steps, harsh reaction conditions, pollution, high cost, etc., are not suitable for industrial mass production

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The production technology of chlorcyclizine hydrochloride comprises the following steps:

[0024] (1) bromination reaction:

[0025] Add 2.47 mol of the raw material p-chlorobisphenylmethane into the reaction vessel, and heat it to 115°C while stirring. After the temperature is constant, slowly drop bromine under stirring. The molar ratio of the dropped bromine to p-chlorobisphenylmethane is 1 : 1.1, after the dropwise addition of the alkane, the insulation reaction was carried out for 3 hours. After the reaction, the reaction solution was cooled to 35° C., then anhydrous sodium carbonate and anhydrous sodium sulfate were added, p-chlorobisphenylmethane: anhydrous sodium carbonate: anhydrous The mol ratio of sodium sulfate is 20: 1: 1, after stirring, discharge, filter, obtain 621 grams (2.2mol) p-chlorobisphenylmethane bromination product crude product stand-by, it is sealed and preserved;

[0026] (2) Condensation reaction:

[0027] Put 110 grams (1.1mol) of N-methy...

Embodiment 2

[0037] The production technology of chlorcyclizine hydrochloride comprises the following steps:

[0038] (1) bromination reaction:

[0039] Add 24.7 mol of the raw material p-chlorobisphenylmethane into the reaction vessel, and heat it to 118°C while stirring. After the temperature is constant, slowly drop bromine under stirring. The molar ratio of the dropped bromine to p-chlorobisphenylmethane is 1 : (1.25), after the dropwise addition of the alkane, the insulation reaction was carried out for 8 hours. After the reaction, the reaction solution was cooled to 40°C, then anhydrous sodium carbonate and anhydrous sodium sulfate were added, p-chlorobisphenylmethane: anhydrous sodium carbonate: The mol ratio of anhydrous sodium sulfate is 20: 1.5: 1.5, after stirring, discharge, filter, obtain 7060 grams (25mol) p-chlorobisphenylmethane bromination product crude product bromide stand-by, it is sealed and preserved;

[0040] (2) Condensation reaction:

[0041] Put 1250 grams (12.5...

Embodiment 3

[0051] The production technology of chlorcyclizine hydrochloride comprises the following steps:

[0052] (1) bromination reaction:

[0053] Add 247mol of the raw material p-chlorobisphenylmethane into the reaction vessel, add it to the reaction vessel, and heat it to 120°C while stirring. After the temperature is constant, slowly drop bromine under stirring. The ratio is 1:(1.25). After the dropwise addition of alkane, keep the temperature for 12 hours. After the reaction, cool the reaction solution to 4.5°C, then add anhydrous sodium carbonate and anhydrous sodium sulfate, p-chlorobisphenylmethane: Anhydrous sodium carbonate: the mol ratio of anhydrous sodium sulfate is 20: 2: 2, discharge after stirring, filter, obtain 72.07 kilograms (255mol) p-chlorobisphenylmethane bromination product crude product stand-by, it is sealed and preserved;

[0054] (2) Condensation reaction:

[0055] Put 12.75 kg (127.5 mol) of N-methylpiperazine, n-heptane, and anhydrous sodium carbonate i...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the technical field of medicine synthesis and especially relates to a production process of chlorcyclizine hydrochloride. The production process comprises the following steps:a bromination reaction; a condensation reaction; distillation; acid and alkali adjustment; crystallization; refining and purifying; and packaging. The production process has the advantages of simpleprocess, few synthesis steps, cheap and easily available raw materials, mild reaction conditions, strong operability, capacity of realizing continuous production, high total yield and suitability forlarge-scale industrial production. Three recrystallization operations are carried out in the process of refining and purifying, so an impurity content is reduced, the purity of chlorcyclizine hydrochloride reaches relevant weight standards prescribed in Pharmacopeia, and the purity of chlorcyclizine hydrochloride is remarkably improved; and meanwhile, refining yield is improved, and production efficiency can be remarkably improved.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a production process of chlorcyclizine hydrochloride. Background technique [0002] Chlorcyclizine hydrochloride is an antihistamine used for various allergic diseases, especially urticaria, hay fever and allergic rhinitis. Its Chinese aliases: fluvoxamine, maleate, chlorcyclizine hydrochloride, meclizine hydrochloride. Wherein the scientific name is: 1-(4-chloro-benzhydryl)-4-methylpiperazine hydrochloride; the production of chlorcyclizine hydrochloride mostly adopts synthetic methods, but various synthetic methods are prone to occur in the commonly used synthetic methods. Many problems, such as many steps, harsh reaction conditions, pollution, high cost, etc., are not suitable for industrialized mass production. Contents of the invention [0003] The object of the present invention is just to overcome above-mentioned deficiency, the production technology of chlorcyclizine hydr...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/073
CPCC07D295/073Y02P20/54
Inventor 罗会军宋安国程利娜
Owner JIAOZUO FURUITANG PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com